Abstract | OBJECTIVE: To test the hypothesis that over a 4-week treatment period, Nal-Glu GnRH antagonist ([AcD2Nal1, D4ClPhe2, D3Pal3, Arg5, DGlu6 [AA], DAla10] GnRH) at a dose of 200 micrograms/kg per day SC would suppress levels of immunologically active and biologically active LH and FSH more completely than a dose of 100 micrograms/kg per day. DESIGN: Placebo controlled clinical study. SETTING: A university community. SUBJECTS: Thirty normal male volunteers. INTERVENTIONS: We administered Nal-Glu at doses of 0, 100, and 200 micrograms/kg body weight per day in combination with T enanthate, 50 mg IM weekly, to separate groups of men (9 or 10 men per group) for 4 weeks. RESULTS: Serum levels of immunologically active and biologically active gonadotropins were suppressed similarly in both groups of men who received Nal-Glu; this suppression was significantly greater than in the men who received placebo + T. Local side effects were more severe in the Nal-Glu 200 micrograms/kg per day group. CONCLUSIONS: Administration of Nal-Glu in combination with T suppresses gonadotropins more completely than does T alone, but at doses > 100 micrograms/kg, gonadotropins are not suppressed additionally with larger doses of Nal-Glu. Subjects experienced greater local discomfort and side effects with the higher dosage. These findings suggest that dosages of Nal-Glu of > 100 micrograms/kg per day may have no advantage over the 100-micrograms/kg dose in a male contraceptive regimen.
|
Authors | C J Bagatell, J E Rivier, W J Bremner |
Journal | Fertility and sterility
(Fertil Steril)
Vol. 64
Issue 1
Pg. 139-45
(Jul 1995)
ISSN: 0015-0282 [Print] United States |
PMID | 7789550
(Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)
|
Chemical References |
- Gonadotropins
- LHRH, N-Ac-2-Nal(1)-4-Cl-Phe(2)-3-Pal(3)-Arg(5)-Glu(6)-AlaNH2(10)-
- Gonadotropin-Releasing Hormone
- Testosterone
- testosterone enanthate
- Luteinizing Hormone
|
Topics |
- Adult
- Biological Assay
- Dose-Response Relationship, Drug
- Drug Synergism
- Fluoroimmunoassay
- Gonadotropin-Releasing Hormone
(adverse effects, analogs & derivatives, antagonists & inhibitors, pharmacology)
- Gonadotropins
(blood)
- Humans
- Luteinizing Hormone
(blood)
- Male
- Radioimmunoassay
- Testosterone
(analogs & derivatives, blood, pharmacology)
|